CN111698995B - 三炔连接剂和使用方法 - Google Patents
三炔连接剂和使用方法 Download PDFInfo
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- CN111698995B CN111698995B CN201980013763.0A CN201980013763A CN111698995B CN 111698995 B CN111698995 B CN 111698995B CN 201980013763 A CN201980013763 A CN 201980013763A CN 111698995 B CN111698995 B CN 111698995B
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- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/06—Phosphorus compounds without P—C bonds
- C07F9/22—Amides of acids of phosphorus
- C07F9/24—Esteramides
- C07F9/2404—Esteramides the ester moiety containing a substituent or a structure which is considered as characteristic
- C07F9/2416—Esteramides the ester moiety containing a substituent or a structure which is considered as characteristic of cycloaliphatic alcohols
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
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- A—HUMAN NECESSITIES
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- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
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- A61K47/545—Heterocyclic compounds
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- A—HUMAN NECESSITIES
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- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/548—Phosphates or phosphonates, e.g. bone-seeking
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- A—HUMAN NECESSITIES
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- A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
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- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C205/00—Compounds containing nitro groups bound to a carbon skeleton
- C07C205/39—Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by esterified hydroxy groups
- C07C205/42—Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by esterified hydroxy groups having nitro groups or esterified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
- C07C205/43—Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by esterified hydroxy groups having nitro groups or esterified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton to carbon atoms of the same non-condensed six-membered aromatic ring or to carbon atoms of six-membered aromatic rings being part of the same condensed ring system
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- C07C205/00—Compounds containing nitro groups bound to a carbon skeleton
- C07C205/49—Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by carboxyl groups
- C07C205/57—Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by carboxyl groups having nitro groups and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
- C07C205/59—Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by carboxyl groups having nitro groups and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton the carbon skeleton being further substituted by singly-bound oxygen atoms
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- C07C233/16—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
- C07C233/17—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
- C07C233/19—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a saturated carbon skeleton containing rings
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- C—CHEMISTRY; METALLURGY
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- C07C233/57—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings
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- C07C233/82—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
- C07C233/83—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom of an acyclic saturated carbon skeleton
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- C—CHEMISTRY; METALLURGY
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- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
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- C07C235/32—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
- C07C235/34—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
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- C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
- C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
- C07C237/22—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
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- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
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- C—CHEMISTRY; METALLURGY
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- C07H21/00—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
- C07H21/02—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical
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- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
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- C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
- C12N15/09—Recombinant DNA-technology
- C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
- C12N15/113—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing
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- C07C2602/36—Systems containing two condensed rings the rings having more than two atoms in common
- C07C2602/38—Systems containing two condensed rings the rings having more than two atoms in common the bicyclo ring system containing five carbon atoms
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Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202510149001.0A CN120247964A (zh) | 2018-02-17 | 2019-02-15 | 三炔连接剂和使用方法 |
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862631683P | 2018-02-17 | 2018-02-17 | |
| US62/631683 | 2018-02-17 | ||
| US201862646739P | 2018-03-22 | 2018-03-22 | |
| US62/646739 | 2018-03-22 | ||
| US201862663763P | 2018-04-27 | 2018-04-27 | |
| US62/663763 | 2018-04-27 | ||
| US201962790300P | 2019-01-09 | 2019-01-09 | |
| US62/790300 | 2019-01-09 | ||
| PCT/US2019/018232 WO2019161213A1 (en) | 2018-02-17 | 2019-02-15 | Trialkyne linking agents and methods of use |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202510149001.0A Division CN120247964A (zh) | 2018-02-17 | 2019-02-15 | 三炔连接剂和使用方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN111698995A CN111698995A (zh) | 2020-09-22 |
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| CA3120580A1 (en) | 2019-01-09 | 2020-07-16 | Arrowhead Pharmaceuticals, Inc. | Rnai agents for inhibiting expression of hif-2 alpha (epas1), compositions thereof, and methods of use |
| AU2020285639A1 (en) | 2019-05-24 | 2021-12-23 | Empirico Inc. | Treatment of angiopoietin like 7 (ANGPTL7) related diseases |
| JP7672394B2 (ja) * | 2019-09-03 | 2025-05-07 | アークトゥラス・セラピューティクス・インコーポレイテッド | 治療的に活性な複合体のアシアロ糖タンパク質受容体媒介送達 |
| WO2022056266A2 (en) * | 2020-09-11 | 2022-03-17 | Arrowhead Pharmaceuticals, Inc. | Rnai agents for inhibiting expression of dux4, compositions thereof, and methods of use |
| CA3189071A1 (en) * | 2020-09-11 | 2022-03-17 | Xiaokai Li | Skeletal muscle delivery platforms and methods of use |
| MX2023011909A (es) | 2021-04-08 | 2023-10-18 | Arrowhead Pharmaceuticals Inc | Agentes de rnai para inhibir la expresion del receptor para productos finales de glicacion avanzada, composiciones de estos y metodos de uso. |
| CN117858949A (zh) | 2021-05-28 | 2024-04-09 | 箭头药业股份有限公司 | 用于抑制粘蛋白5AC(MUC5AC)的表达的RNAi试剂、其组合物及其使用方法 |
| CN113956206B (zh) * | 2021-10-25 | 2023-04-28 | 深圳湾实验室坪山生物医药研发转化中心 | 一种用于修饰蛋白质赖氨酸残基的探针及其制备方法 |
| KR20240163743A (ko) | 2022-03-28 | 2024-11-19 | 엠피리코 인크. | 변형된 올리고뉴클레오티드 |
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| TW202440163A (zh) * | 2022-12-14 | 2024-10-16 | 美商艾拉倫製藥股份有限公司 | 用於肝外遞送之α-V β-6(αvβ6)整合素配體 |
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| CN120309684A (zh) * | 2024-01-15 | 2025-07-15 | 武汉人福创新药物研发中心有限公司 | 靶向化合物及其用途 |
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| WO2015107115A1 (en) * | 2014-01-15 | 2015-07-23 | Basf Se | Saccharide-modified nucleic acid molecules |
| WO2018013525A1 (en) * | 2016-07-11 | 2018-01-18 | Translate Bio Ma, Inc. | Nucleic acid conjugates and uses thereof |
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| WO2007125429A2 (en) * | 2006-04-28 | 2007-11-08 | Centre National De La Recherche Scientifique | Method for the synthesis of triazole- containing oligonucleotide derivatives |
| GB201313201D0 (en) * | 2013-07-24 | 2013-09-04 | Univ East Anglia | Virus Detection |
| EP3294810A4 (en) * | 2015-05-12 | 2019-01-02 | Blinkbio Inc. | Silicon based drug conjugates and methods of using same |
| TN2019000308A1 (en) * | 2017-07-06 | 2021-05-07 | Arrowhead Pharmaceuticals Inc | RNAi AGENTS FOR INHIBITING EXPRESSION OF ALPHA-ENaC AND METHODS OF USE |
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| WO2015107115A1 (en) * | 2014-01-15 | 2015-07-23 | Basf Se | Saccharide-modified nucleic acid molecules |
| WO2018013525A1 (en) * | 2016-07-11 | 2018-01-18 | Translate Bio Ma, Inc. | Nucleic acid conjugates and uses thereof |
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| Automated Solid-Phase Click Synthesis of Oligonucleotide Conjugates: From Small Molecules to Diverse N-Acetylgalactosamine Clusters;Valentina M. Farzan 等;《Bioconjugate Chem.》;第28卷(第10期);第2599-2607页 * |
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| AU2019220739A1 (en) | 2020-09-03 |
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| CN120247964A (zh) | 2025-07-04 |
| EP3752166A1 (en) | 2020-12-23 |
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